Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2025;31(31):2481-2503.
doi: 10.2174/0113816128357976250122042633.

Targeting the PI3K Pathway: Advancements and Achievements in Breast Cancer Therapy

Basavana Gowda Hosur Dinesh  1 , Sunil Kumar Bandral  1 , Nandini Markuli Sadashivappa  1 , Srinivas Ganjipete  1 , Damodar Nayak Ammunje  2 , Selvaraj Kunjiappan  3 , Panneerselvam Theivendren  4 , Judy Jays  1 , Parasuraman Pavadai  1
Affiliations
Review

Targeting the PI3K Pathway: Advancements and Achievements in Breast Cancer Therapy

Basavana Gowda Hosur Dinesh et al. Curr Pharm Des. 2025.

Abstract

Breast cancer is a complex disease caused by the aberrant and unchecked proliferation of breast cells, which leads to the development of tumours. In various types of cancer, the Phosphoinositide 3- kinase/Protein kinase B (PKB, also known as Akt (PI3K/Akt) signalling pathway, is essential for controlling cell survival, metastasis, and metabolism. Currently, marketed PI3K inhibitors for treating breast cancer face several issues, including toxicity, resistance, etc. Significant efforts have been made to develop synthetic and repurposed inhibitor drugs to target PI3K, which are now being tested in clinical trials. Developed synthetic PI3K inhibitors have been reported to have better results in clinical trials in the suppression of tumors. This review article mainly focuses on the PI3K pathway at the cellular and molecular level, the development of PI3K inhibitors, and their clinical trials. Biomarkers, marine drugs, synthetic drugs, and repurposed drugs to treat breast cancer are also discussed, followed by mutational changes in PI3K and the resistance mechanism involved in PI3K inhibitors.

Keywords: Breast cancer; PI3K inhibitors; biomarkers; clinical trials; mutation; resistance; synthetic drugs..

PubMed Disclaimer

References

    1. Cooper G.M.; Hausman R.E.; The development and causes of cancer. The Cell: A Molecular Approach 2000
    1. Surya C.; Lakshminarayana A.B.V.; Ramesh S.H.; Kunjiappan S.; Theivendren P.; Santhana Krishna Kumar A.; Ammunje D.N.; Pavadai P.; Advancements in breast cancer therapy: The promise of copper nanoparticles. J Trace Elem Med Biol 2024,86,127526 - DOI - PubMed
    1. Makker V.; Recio F.O.; Ma L.; Matulonis U.A.; Lauchle J.O.; Parmar H.; Gilbert H.N.; Ware J.A.; Zhu R.; Lu S.; Huw L.Y.; Wang Y.; Koeppen H.; Spoerke J.M.; Lackner M.R.; Aghajanian C.A.; A multicenter, single‐arm, open‐label, phase 2 study of apitolisib (GDC‐0980) for the treatment of recurrent or persistent endometrial carcinoma (MAGGIE study). Cancer 2016,122(22),3519-3528 - DOI - PubMed
    1. Kalimuthu A.K.; Panneerselvam T.; Pavadai P.; Pandian S.R.K.; Sundar K.; Murugesan S.; Ammunje D.N.; Kumar S.; Arunachalam S.; Kunjiappan S.; Pharmacoinformatics-based investigation of bioactive compounds of Rasam (South Indian recipe) against human cancer. Sci Rep 2021,11(1),21488 - DOI - PubMed
    1. Hu K.; Lou L.; Tian W.; Pan T.; Ye J.; Zhang S.; The outcome of breast cancer is associated with national human development index and health system attainment. PLoS One 2016,11(7),e0158951 - DOI - PubMed

MeSH terms

Substances

LinkOut - more resources